Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action

[Display omitted] A series of novel STAT3 inhibitors consisting of Michael acceptor has been identified through assays of the focused in-house library. In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In particular, analog 6 revealed pr...

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Published in:Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5444-5448
Main Authors: Kim, Kyeojin, Kim, Su-Jung, Han, Young Taek, Hong, Sung-Jun, An, Hongchan, Chang, Dong-Jo, Kim, Taewoo, Lim, Bumhee, Lee, Jeeyeon, Surh, Young-Joon, Suh, Young-Ger
Format: Article
Language:English
Subjects:
Antitumor
Apoptosis
Breast cancer
Breast Neoplasms - drug therapy
Cell Line, Tumor
Cell Survival - drug effects
Female
HeLa Cells
Humans
Immunoblotting
Phosphorylation - drug effects
Signal Transduction - drug effects
Small molecule inhibitors
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
STAT3
STAT3 Transcription Factor - antagonists & inhibitors
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cited_by cdi_FETCH-LOGICAL-c426t-4397632f68253d1739fce79069872088db77f2f3405e5d617fa168f6a59cc5dc3
cites cdi_FETCH-LOGICAL-c426t-4397632f68253d1739fce79069872088db77f2f3405e5d617fa168f6a59cc5dc3
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container_issue 22
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container_title Bioorganic & medicinal chemistry letters
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creator Kim, Kyeojin
Kim, Su-Jung
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Kim, Taewoo
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Surh, Young-Joon
Suh, Young-Ger
description [Display omitted] A series of novel STAT3 inhibitors consisting of Michael acceptor has been identified through assays of the focused in-house library. In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In particular, analog 6 revealed promising STAT3 inhibitory activity in HeLa cell lines. The analog also exhibited selective inhibition of STAT3 phosphorylation without affecting STAT1 phosphorylation and cytostatic effect in human breast epithelial cells (MCF10A-ras), which supports cancer cell-specific inhibitory properties.
doi_str_mv 10.1016/j.bmcl.2015.07.063
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In addition, their mode of action and structural feature responsible for the STAT3 inhibition were investigated. In particular, analog 6 revealed promising STAT3 inhibitory activity in HeLa cell lines. 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source ScienceDirect Journals
subjects Antitumor
Apoptosis
Breast cancer
Breast Neoplasms - drug therapy
Cell Line, Tumor
Cell Survival - drug effects
Female
HeLa Cells
Humans
Immunoblotting
Phosphorylation - drug effects
Signal Transduction - drug effects
Small molecule inhibitors
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
STAT3
STAT3 Transcription Factor - antagonists & inhibitors
title Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action
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